Metabolic pathways are upregulated in cancer cells to promote their growth and proliferation. The evidence pointing to the requirement of the amino acid serine in tumorigenesis is overwhelming. Serine is required for a large number of anabolic processes including amino acid and lipid biosynthesis. The enzyme 3-phosphoglycerate dehydrogenase (PHGDH) catalyzes the first committed step in cellular serine biosynthesis and is overexpressed in cancer cell lines and tumors.
CBR-5884 – a selective small molecule inhibitor of PHGDH recently discovered
Very recently, in a joint effort, the laboratories of Cantley, Lyssiotis and Lairson reported the discovery of a selective small molecule inhibitor of PHGDH designated CBR-5884 (1).
This compound inhibits serine biosynthesis in cancer cells and displays selective cytotoxicity to tumor cell lines overexpressing PHGDH. The identification of CBR-5884 as a drug-like inhibitor of serine biosynthesis is a breakthrough in targeting metabolism in cancer drug development. It is an important compound which provides proof of concept that PHGDH is a viable target, and may represent a lead molecule for the development of more potent analogs. In the mean time it serves as an important new tool compound for the study of cellular serine metabolism.
CBR-5884 is available as a research tool from Focus Biomolecules and tebu-bio
Focus Biomolecules has been the first company to make this promising compound available to the market for cancer research studies.
CBR-5884 (cat. nr 10-1588) can be purchased in Europe through tebu-bio. The compound is available in standard sizes (5 mg & 25 mg) or in bulk amounts (upon request).
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(1) Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers. E Mullarky et al. Proc. Acad. Natl. Sci. USA 2016 113:1778
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